25 Amino Acids 26 Chemicals 27 – 35 Nutritionals 36 – 52
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Specifications of Approved Drug Compound Library
Annexure-I : Specifications of Approved drug compound library The compounds should be structurally diverse, medicinally active, and cell permeable Compounds should have rich documentation with structure, Target, Activity and IC50 should be known Compounds which are supplied should have been validated by NMR and HPLC to ensure high purity Each compound should be supplied as 10mM solution in DMSO and at least 100µl of each compound should be supplied. Compounds should be supplied in screw capped vial arranged as 96 well plate format. -
Design Novel Dual Agonists for Treating Type-2 Diabetes by Targeting Peroxisome Proliferator-Activated Receptors with Core Hopping Approach
Design Novel Dual Agonists for Treating Type-2 Diabetes by Targeting Peroxisome Proliferator-Activated Receptors with Core Hopping Approach Ying Ma1., Shu-Qing Wang1,3*., Wei-Ren Xu2, Run-Ling Wang1*, Kuo-Chen Chou3 1 Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China, 2 Tianjin Institute of Pharmaceutical Research (TIPR), Tianjin, China, 3 Gordon Life Science Institute, San Diego, California, United States of America Abstract Owing to their unique functions in regulating glucose, lipid and cholesterol metabolism, PPARs (peroxisome proliferator- activated receptors) have drawn special attention for developing drugs to treat type-2 diabetes. By combining the lipid benefit of PPAR-alpha agonists (such as fibrates) with the glycemic advantages of the PPAR-gamma agonists (such as thiazolidinediones), the dual PPAR agonists approach can both improve the metabolic effects and minimize the side effects caused by either agent alone, and hence has become a promising strategy for designing effective drugs against type-2 diabetes. In this study, by means of the powerful ‘‘core hopping’’ and ‘‘glide docking’’ techniques, a novel class of PPAR dual agonists was discovered based on the compound GW409544, a well-known dual agonist for both PPAR-alpha and PPAR- gamma modified from the farglitazar structure. It was observed by molecular dynamics simulations that these novel agonists not only possessed the same function as GW409544 did in activating PPAR-alpha and PPAR-gamma, but also had more favorable conformation for binding to the two receptors. It was further validated by the outcomes of their ADME (absorption, distribution, metabolism, and excretion) predictions that the new agonists hold high potential to become drug candidates. -
Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany). -
Next-Generation Sequencing Identification and Characterization
Next-generation sequencing identification and characterization of microsatellite markers in Aconitum austrokoreense Koidz., an endemic and endangered medicinal plant of Korea Y.-E. Yun, J.-N. Yu, G.H. Nam, S.-A. Ryu, S. Kim, K. Oh and C.E. Lim National Institute of Biological Resources, Environmental Research Complex, Incheon, Korea Corresponding author: C.E. Lim E-mail: [email protected] Genet. Mol. Res. 14 (2): 4812-4817 (2015) Received June 11, 2014 Accepted October 29, 2014 Published May 11, 2015 DOI http://dx.doi.org/10.4238/2015.May.11.13 ABSTRACT. We used next-generation sequencing to develop 9 novel microsatellite markers in Aconitum austrokoreense, an endemic and endangered medicinal plant in Korea. Owing to its very limited distribution, over-harvesting for traditional medicinal purposes, and habitat loss, the natural populations are dramatically declining in Korea. All novel microsatellite markers were successfully genotyped using 64 samples from two populations (Mt. Choejeong, Gyeongsangbuk- do and Ungseokbong, Gyeongsangnam-do) of Gyeongsang Province. The number of alleles ranged from 2 to 7 per locus in each population. Observed and expected heterozygosities ranged from 0.031 to 0.938 and from 0.031 to 0.697, respectively. The novel markers will be valuable tools for assessing the genetic diversity of A. austrokoreense and for germplasm conservation of this endangered species. Key words: Aconitum austrokoreense; Microsatellite marker; Endemic and endangered medicinal plant, Next-generation sequencing; Genetic diversity Genetics and Molecular Research 14 (2): 4812-4817 (2015) ©FUNPEC-RP www.funpecrp.com.br Novel microsatellite markers in A. austrokoreense 4813 INTRODUCTION Aconitum austrokoreense Koidz. -
Us 2018 / 0296525 A1
UN US 20180296525A1 ( 19) United States (12 ) Patent Application Publication (10 ) Pub. No. : US 2018/ 0296525 A1 ROIZMAN et al. ( 43 ) Pub . Date: Oct. 18 , 2018 ( 54 ) TREATMENT OF AGE - RELATED MACULAR A61K 38 /1709 ( 2013 .01 ) ; A61K 38 / 1866 DEGENERATION AND OTHER EYE (2013 . 01 ) ; A61K 31/ 40 ( 2013 .01 ) DISEASES WITH ONE OR MORE THERAPEUTIC AGENTS (71 ) Applicant: MacRegen , Inc ., San Jose , CA (US ) (57 ) ABSTRACT ( 72 ) Inventors : Keith ROIZMAN , San Jose , CA (US ) ; The present disclosure provides therapeutic agents for the Martin RUDOLF , Luebeck (DE ) treatment of age - related macular degeneration ( AMD ) and other eye disorders. One or more therapeutic agents can be (21 ) Appl. No .: 15 /910 , 992 used to treat any stages ( including the early , intermediate ( 22 ) Filed : Mar. 2 , 2018 and advance stages ) of AMD , and any phenotypes of AMD , including geographic atrophy ( including non -central GA and Related U . S . Application Data central GA ) and neovascularization ( including types 1 , 2 and 3 NV ) . In certain embodiments , an anti - dyslipidemic agent ( 60 ) Provisional application No . 62/ 467 ,073 , filed on Mar . ( e . g . , an apolipoprotein mimetic and / or a statin ) is used 3 , 2017 . alone to treat or slow the progression of atrophic AMD Publication Classification ( including early AMD and intermediate AMD ) , and / or to (51 ) Int. CI. prevent or delay the onset of AMD , advanced AMD and /or A61K 31/ 366 ( 2006 . 01 ) neovascular AMD . In further embodiments , two or more A61P 27 /02 ( 2006 .01 ) therapeutic agents ( e . g ., any combinations of an anti - dys A61K 9 / 00 ( 2006 . 01 ) lipidemic agent, an antioxidant, an anti- inflammatory agent, A61K 31 / 40 ( 2006 .01 ) a complement inhibitor, a neuroprotector and an anti - angio A61K 45 / 06 ( 2006 .01 ) genic agent ) that target multiple underlying factors of AMD A61K 38 / 17 ( 2006 .01 ) ( e . -
(12) United States Patent (10) Patent No.: US 9,314.465 B2 Brew Et Al
US009314465B2 (12) United States Patent (10) Patent No.: US 9,314.465 B2 Brew et al. (45) Date of Patent: *Apr. 19, 2016 (54) DRUG COMBINATIONS AND USES IN 2008.0003280 A1 1/2008 Levine et al. ................. 424/456 TREATING A COUGHING CONDITION 2008/O176955 A1 7/2008 Hecket al. 2008, 0220078 A1 9, 2008 Morton et al. (71) Applicant: Infirst Healthcare Limited 2009, O136427 A1 5/2009 Croft et al. 2009, O220594 A1 9, 2009 Field (72) Inventors: John Brew, London (GB); Robin Mark 2012/O128738 A1 5, 2012 Brew et al. Bannister, London (GB) 2012fO252824 A1 10/2012 Brew et al. (73) Assignee: Infirst Healthcare Limited, London FOREIGN PATENT DOCUMENTS (GB) CN 1593451 3, 2005 CN 101024.014 A 8, 2007 (*) Notice: Subject to any disclaimer, the term of this CN 101112383 B 5, 2010 patent is extended or adjusted under 35 DE 4420708 A1 12, 1995 U.S.C. 154(b) by 0 days. EP 2050435 B1 4/2009 GB 2114001 A 8, 1983 This patent is Subject to a terminal dis GB 2284761 A 6, 1995 claimer. GB 2424.185 B 9, 2006 GB 2442828 A 4/2008 JP 62-249924 A 10, 1987 (21) Appl. No.: 14/287,014 JP H1O-316568 A 12/1998 JP 2001-518928 A 10, 2001 (22) Filed: May 24, 2014 JP 200219.3839. A T 2002 JP 2003-012514 A 1, 2003 (65) Prior Publication Data JP 20030552.58 A 2, 2003 JP 2003128549 A 5, 2003 US 2014/O256750 A1 Sep. 11, 2014 JP 2003-321357 A 11, 2003 JP 2005-516917 A 6, 2005 JP 2008O31146 A 2, 2008 Related U.S. -
ACCP Guideline: Diagnosis and Management of Cough
Diagnosis and Management of Cough Executive Summary ACCP Evidence-Based Clinical Practice Guidelines Richard S. Irwin, MD, FCCP, Chair; Michael H. Baumann, MD, FCCP (HSP Liaison); Donald C. Bolser, PhD; Louis-Philippe Boulet, MD, FCCP (CTS Representative); Sidney S. Braman, MD, FCCP; Christopher E. Brightling, MBBS, FCCP; Kevin K. Brown, MD, FCCP; Brendan J. Canning, PhD; Anne B. Chang, MBBS, PhD; Peter V. Dicpinigaitis, MD, FCCP; Ron Eccles, DSc; W. Brendle Glomb, MD, FCCP; Larry B. Goldstein, MD; LeRoy M. Graham, MD, FCCP; Frederick E. Hargreave, MD; Paul A. Kvale, MD, FCCP; Sandra Zelman Lewis, PhD; F. Dennis McCool, MD, FCCP; Douglas C. McCrory, MD, MHSc; Udaya B.S. Prakash, MD, FCCP; Melvin R. Pratter, MD, FCCP; Mark J. Rosen, MD, FCCP; Edward Schulman, MD, FCCP (ATS Representative); John Jay Shannon, MD, FCCP (ACP Representative); Carol Smith Hammond, PhD; and Susan M. Tarlo, MBBS, FCCP (CHEST 2006; 129:1S–23S) Abbreviations: ACE ϭ angiotensin-converting enzyme; ACP ϭ American College of Physicians; A/D ϭ antihistamine/ decongestant; ATS ϭ American Thoracic Society; BPC ϭ bronchoprovocation challenge; CTS ϭ Canadian Thoracic Society; DPB ϭ diffuse panbronchiolitis; dTap ϭ acellular pertussis; FEES ϭ fiberoptic endoscopic evaluation of swallowing; GERD ϭ gastroesophageal reflux disease; HRCT ϭ high-resolution CT; HSP ϭ Health & Psychosocial Instruments; IBD ϭ inflammatory bowel disease; ICS ϭ inhaled corticosteroid; ILD ϭ interstitial lung disease; NAEB ϭ nonasthmatic eosinophilic bronchitis; NSCLC ϭ non-small cell lung cancer; SLP ϭ speech-language pathol- ogist; TB ϭ tuberculosis; UACS ϭ upper airway cough syndrome; URI ϭ upper respiratory infection; VC ϭ voluntary cough; VSE ϭ videofluoroscopic swallow evaluation ecognition of the importance of cough in clinical (3) updates and expands, when appropriate, all pre- R medicine was the impetus for the original evi- vious sections; and (4) adds new sections with topics dence-based consensus panel report on “Managing that were not previously covered. -
The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development
International Journal of Molecular Sciences Review The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development Fan Hong 1,2, Pengfei Xu 1,*,† and Yonggong Zhai 1,2,* 1 Beijing Key Laboratory of Gene Resource and Molecular Development, College of Life Sciences, Beijing Normal University, Beijing 100875, China; [email protected] 2 Key Laboratory for Cell Proliferation and Regulation Biology of State Education Ministry, College of Life Sciences, Beijing Normal University, Beijing 100875, China * Correspondence: [email protected] (P.X.); [email protected] (Y.Z.); Tel.: +86-156-005-60991 (P.X.); +86-10-5880-6656 (Y.Z.) † Current address: Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15213, USA. Received: 22 June 2018; Accepted: 24 July 2018; Published: 27 July 2018 Abstract: Peroxisome proliferator-activated receptors (PPARs) are a well-known pharmacological target for the treatment of multiple diseases, including diabetes mellitus, dyslipidemia, cardiovascular diseases and even primary biliary cholangitis, gout, cancer, Alzheimer’s disease and ulcerative colitis. The three PPAR isoforms (α, β/δ and γ) have emerged as integrators of glucose and lipid metabolic signaling networks. Typically, PPARα is activated by fibrates, which are commonly used therapeutic agents in the treatment of dyslipidemia. The pharmacological activators of PPARγ include thiazolidinediones (TZDs), which are insulin sensitizers used in the treatment of type 2 diabetes mellitus (T2DM), despite some drawbacks. In this review, we summarize 84 types of PPAR synthetic ligands introduced to date for the treatment of metabolic and other diseases and provide a comprehensive analysis of the current applications and problems of these ligands in clinical drug discovery and development. -
Research Article to Probe Full and Partial Activation
Hindawi PPAR Research Volume 2020, Article ID 5314187, 24 pages https://doi.org/10.1155/2020/5314187 Research Article To Probe Full and Partial Activation of Human Peroxisome Proliferator-Activated Receptors by Pan-Agonist Chiglitazar Using Molecular Dynamics Simulations Holli-Joi Sullivan,1 Xiaoyan Wang,2,3 Shaina Nogle,1 Siyan Liao,1,4 and Chun Wu 1 1College of Science and Mathematics, Rowan University, Glassboro, NJ 08028, USA 2School of Radiology, Taishan Medical University, Tai’an, Shandong 271016, China 3Medical School, Southeast University, Nanjing 210009, China 4Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou 511436, China Correspondence should be addressed to Chun Wu; [email protected] Received 13 January 2020; Revised 25 February 2020; Accepted 3 March 2020; Published 1 April 2020 Academic Editor: Tom Hsun-Wei Huang Copyright © 2020 Holli-Joi Sullivan et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Chiglitazar is a promising new-generation insulin sensitizer with low reverse effects for the treatment of type II diabetes mellitus (T2DM) and has shown activity as a nonselective pan-agonist to the human peroxisome proliferator-activated receptors (PPARs) (i.e., full activation of PPARγ and a partial activation of PPARα and PPARβ/δ). Yet, it has no high-resolution complex structure with PPARs and its detailed interactions and activation mechanism remain unclear. In this study, we docked chiglitazar into three experimentally resolved crystal structures of hPPAR subtypes, PPARα, PPARβ/δ, and PPARγ, followed by 3 μs molecular dynamics simulations for each system. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
General Pharmacology
GENERAL PHARMACOLOGY Winners of “Nobel” prize for their contribution to pharmacology Year Name Contribution 1923 Frederick Banting Discovery of insulin John McLeod 1939 Gerhard Domagk Discovery of antibacterial effects of prontosil 1945 Sir Alexander Fleming Discovery of penicillin & its purification Ernst Boris Chain Sir Howard Walter Florey 1952 Selman Abraham Waksman Discovery of streptomycin 1982 Sir John R.Vane Discovery of prostaglandins 1999 Alfred G.Gilman Discovery of G proteins & their role in signal transduction in cells Martin Rodbell 1999 Arvid Carlson Discovery that dopamine is neurotransmitter in the brain whose depletion leads to symptoms of Parkinson’s disease Drug nomenclature: i. Chemical name ii. Non-proprietary name iii. Proprietary (Brand) name Source of drugs: Natural – plant /animal derivatives Synthetic/semisynthetic Plant Part Drug obtained Pilocarpus microphyllus Leaflets Pilocarpine Atropa belladonna Atropine Datura stramonium Physostigma venenosum dried, ripe seed Physostigmine Ephedra vulgaris Ephedrine Digitalis lanata Digoxin Strychnos toxifera Curare group of drugs Chondrodendron tomentosum Cannabis indica (Marijuana) Various parts are used ∆9Tetrahydrocannabinol (THC) Bhang - the dried leaves Ganja - the dried female inflorescence Charas- is the dried resinous extract from the flowering tops & leaves Papaver somniferum, P album Poppy seed pod/ Capsule Natural opiates such as morphine, codeine, thebaine Cinchona bark Quinine Vinca rosea periwinkle plant Vinca alkaloids Podophyllum peltatum the mayapple -
Mucoactive Agents for Airway Mucus Hypersecretory Diseases
Mucoactive Agents for Airway Mucus Hypersecretory Diseases Duncan F Rogers PhD FIBiol Introduction Sputum Profile of Airway Inflammation and Mucus Hypersecretory Phenotype in Asthma, COPD, and CF Which Aspect of Airway Mucus Hypersecretion to Target? Theoretical Requirements for Effective Therapy of Airway Mucus Hypersecretion Current Recommendations for Clinical Use of Mucolytic Drugs Mucoactive Drugs N-Acetylcysteine: How Does it Work? Does it Work? Dornase Alfa Hypertonic Saline Surfactant Analysis Summary Airway mucus hypersecretion is a feature of a number of severe respiratory diseases, including asthma, chronic obstructive pulmonary disease (COPD), and cystic fibrosis (CF). However, each disease has a different airway inflammatory response, with consequent, and presumably linked, mucus hypersecretory phenotype. Thus, it is possible that optimal treatment of the mucus hyper- secretory element of each disease should be disease-specific. Nevertheless, mucoactive drugs are a longstanding and popular therapeutic option, and numerous compounds (eg, N-acetylcysteine, erdosteine, and ambroxol) are available for clinical use worldwide. However, rational recommen- dation of these drugs in guidelines for management of asthma, COPD, or CF has been hampered by lack of information from well-designed clinical trials. In addition, the mechanism of action of most of these drugs is unknown. Consequently, although it is possible to categorize them according to putative mechanisms of action, as expectorants (aid and/or induce cough), mucolytics (thin